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4v24

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Revision as of 11:15, 26 February 2020

Sphingosine kinase 1 in complex with PF-543

Structural highlights

4v24 is a 2 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	,
Activity:	Sphinganine kinase, with EC number 2.7.1.91
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[SPHK1_HUMAN] Catalyzes the phosphorylation of sphingosine to form sphingosine 1-phosphate (SPP), a lipid mediator with both intra- and extracellular functions. Also acts on D-erythro-sphingosine and to a lesser extent sphinganine, but not other lipids, such as D,L-threo-dihydrosphingosine, N,N-dimethylsphingosine, diacylglycerol, ceramide, or phosphatidylinositol.^[1]

Publication Abstract from PubMed

The most potent inhibitor of Sphingosine Kinase 1 (SPHK1) so far identified is PF-543. The crystal structure of SPHK1 in complex with inhibitor PF-543 to 1.8 A resolution reveals the inhibitor bound in a bent conformation analogous to that expected of a bound sphingosine substrate but with a rotated head group. The structural data presented will aid in the design of SPHK1 and SPHK2 inhibitors with improved properties.

Crystal Structure of Sphingosine Kinase 1 with PF-543.,Wang J, Knapp S, Pyne NJ, Pyne S, Elkins JM ACS Med Chem Lett. 2014 Oct 27;5(12):1329-33. doi: 10.1021/ml5004074. eCollection, 2014 Dec 11. PMID:25516793^[2]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Alvarez SE, Harikumar KB, Hait NC, Allegood J, Strub GM, Kim EY, Maceyka M, Jiang H, Luo C, Kordula T, Milstien S, Spiegel S. Sphingosine-1-phosphate is a missing cofactor for the E3 ubiquitin ligase TRAF2. Nature. 2010 Jun 24;465(7301):1084-8. doi: 10.1038/nature09128. PMID:20577214 doi:10.1038/nature09128
↑ Wang J, Knapp S, Pyne NJ, Pyne S, Elkins JM. Crystal Structure of Sphingosine Kinase 1 with PF-543. ACS Med Chem Lett. 2014 Oct 27;5(12):1329-33. doi: 10.1021/ml5004074. eCollection, 2014 Dec 11. PMID:25516793 doi:http://dx.doi.org/10.1021/ml5004074

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/4v24"

@@ Line 1: / Line 1: @@
 ==Sphingosine kinase 1 in complex with PF-543==
-<StructureSection load='4v24' size='340' side='right' caption='[[4v24]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
+<StructureSection load='4v24' size='340' side='right'caption='[[4v24]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
 == Structural highlights ==
 <table><tr><td colspan='2'>[[4v24]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4V24 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4V24 FirstGlance]. <br>
@@ Line 24: / Line 24: @@
 </StructureSection>
 [[Category: Human]]
+[[Category: Large Structures]]
 [[Category: Sphinganine kinase]]
 [[Category: Bountra, C]]

4v24

From Proteopedia

Revision as of 11:15, 26 February 2020

Sphingosine kinase 1 in complex with PF-543

Structural highlights

Function

Publication Abstract from PubMed

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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